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US4454139A
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α2 -Adrenoceptor antagonistic benzoquinolizines
Assignee: John Wyeth and Brother Ltd
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Filing: 1982-09-09
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Granted: 1984-06-12
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Expires: 2002-09-09
Abstract
Abstract The invention concerns benzoquinolizines of formula ##STR1## and their acid addition salts. In the formula R 7 is lower alkyl or a phenyl or naphthyl radical optionally substituted with specified substituents and R 8 is methyl or ethyl. The compounds possess high α 2 (presynaptic) adrenoceptor antagonistic activity and a good α 2 /α 1 antagonistic selectivity.
Inventors
- 👤 Terence J. Ward
- 👤 John L. Archibald
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 10:27
CPC Classifications
C; C07; C07D; C07D455/00; C07D455/03; C07D455/04; C07D455/06
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
54 words
A compound selected from the group consisting of a benzoquinolizine of the formula ##STR4## and a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is lower alkyl or a phenyl or naphthyl radical optionally substituted by one or more lower alkyl, lower alkoxy or halogen substituents and R 8 is methyl or ethyl.
Claim 2
Dependent Claim
54 words
A compound selected from the group consisting of a benzoquinolizine of the formula ##STR4## and a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is lower alkyl or a phenyl or naphthyl radical optionally substituted by one or more lower alkyl, lower alkoxy or halogen substituents and R 8 is methyl or ethyl.
Claim 3
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)methanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)propan-1-sulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)benzenesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)ethanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
17 words
A compound according to claim 1 which is N-ethyl-N-(1,3,4,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)methanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)toluene-4-sulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-4-methoxybenzenesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-4-chlorobenzenesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 11
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-2-methylbenzenesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 12
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-3,4-dichlorobenzenesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 13
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-n-butanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 14
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-isobutanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 15
Dependent Claim
80 words
A pharmaceutical composition having α 2 -adrenoceptor antagonistic activity comprising an amount effective to antagonise α 2 adrenoceptors of a compound selected from the group consisting of a benzoquinolizine of the formula ##STR5## and a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is lower alkyl or a phenyl or naphthyl radical optionally substituted by one or more lower alkyl, lower alkoxy or halogen substituents and R 8 is methyl or ethyl, in association with a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
80 words
A pharmaceutical composition having α 2 -adrenoceptor antagonistic activity comprising an amount effective to antagonise α 2 adrenoceptors of a compound selected from the group consisting of a benzoquinolizine of the formula ##STR5## and a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is lower alkyl or a phenyl or naphthyl radical optionally substituted by one or more lower alkyl, lower alkoxy or halogen substituents and R 8 is methyl or ethyl, in association with a pharmaceutically acceptable carrier.
Claim 17
Independent Claim
76 words
A method of selectively antagonising α 2 adrenoceptors in warm blooded animals which comprises administering to the animal an effective amount of a compound selected from the group consisting of a benzoquinolizine of the formula ##STR6## and a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is lower alkyl or a phenyl or naphthyl radical optionally substituted by one or more lower alkyl, lower alkoxy or halogen substituents and R 8 is methyl or ethyl.
Claim 18
Independent Claim
76 words
A method of selectively antagonising α 2 adrenoceptors in warm blooded animals which comprises administering to the animal an effective amount of a compound selected from the group consisting of a benzoquinolizine of the formula ##STR6## and a pharmaceutically acceptable acid addition salt thereof, wherein R 7 is lower alkyl or a phenyl or naphthyl radical optionally substituted by one or more lower alkyl, lower alkoxy or halogen substituents and R 8 is methyl or ethyl.
References Cited (Backward Citations)
GB1513824A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-06-12 | 1987-12-12 | 1988-06-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-06-12 | 1991-12-12 | 1992-06-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-06-12 | 1995-12-12 | 1996-06-12 | $7700.00 | Window Closed / Lapsed |